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1) ¸¸¼ºÆó¼â°¢³ì³»Àå, °¡¼º¼öÁ¤Ã¼ ȯÀÚ (°³¹æ°¢ ³ì³»Àå, »ö¼Ò¼º ³ì³»Àå¿¡ ´ëÇÑ ¶óŸ³ëÇÁ·Î½ºÆ®ÀÇ ¿¬±¸ °æÇèÀº ÇÑÁ¤µÇ¾î ÀÖ´Ù. ¶óŸ³ëÇÁ·Î½ºÆ®´Â µ¿°ø¿¡ ¿µÇâÀ» ¹ÌÄ¡Áö ¾ÊÀ¸³ª Æó¼â°¢ ³ì³»ÀåÀÇ ±Þ¼º ¹ßÀÛ, ¿°Áõ¼º, ½Å»ýÇ÷°ü, ¼±Ãµ¼º ³ì³»Àå¿¡ ´ëÇØ ¿¬±¸µÈ ¹Ù ¾øÀ¸¹Ç·Î ÀÌ·¯ÇÑ È¯Àڵ鿡 ´ëÇØ¼´Â ´õ ¸¹Àº °æÇèÀÌ ¾ò¾îÁú ¶§±îÁö ÁÖÀÇÇÏ¿© »ç¿ëµÇ¾î¾ß ÇÑ´Ù.)
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ÀüüÀӽŠ±â°£º°·Î ¿©·¯µî±ÞÀÌ Á¸ÀçÇÒ ¼ö ÀÖÀ¸¸ç °¡Àå À§Çèµµ°¡ ³ôÀº Á¤º¸¸¸ º¸¿©Áý´Ï´Ù. ´Ü, º¹ÇÕÁ¦ÀÇ °æ¿ì ¸ðµç º¹ÇÕÁ¦¼ººÐ¿¡ ´ëÇÑ ÀÓºÎÅõ¿©µî±ÞÀÌ Ç¥½ÃµÈ°ÍÀº Àý´ë ¾Æ´Ï¸ç Ç¥½ÃµÈ°ÍÁß¿¡ °¡Àå À§Çèµµ°¡ ³ôÀº Á¤º¸¸¸ ³ªÅ¸³³´Ï´Ù.
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 FDA : Dµî±Þ
(timolol ÀӽŠ2±â ¶Ç´Â 3±â Åõ¿©½Ã )
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»ó±â ÀÓºÎÅõ¿©¿¡ ´ëÇÑ Á¤º¸´Â Àü»êó¸® µÇ¸é¼ ÀÔ·Â ¿À·ù °¡´É¼ºÀÌ Á¸ÀçÇÕ´Ï´Ù. ¿À·ù °¡´É¼ºÀ» ÃÖ¼ÒÈÇϱâ À§ÇÏ¿© ¸¹Àº ³ë·ÂÀ» ±â¿ïÀ̰í ÀÖÀ¸³ª, ±× Á¤È®¼º¿¡ ´ëÇÏ¿© È®½ÅÀ» µå¸± ¼ö ¾ø½À´Ï´Ù. ÀÌ¿¡ ´ëÇØ ȸ»ç´Â Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù.
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À¯·áÁ¤º¸ÀÔ´Ï´Ù.
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[Á¡¾È¾×] |
| º¸°ü»ó ÁÖÀÇ |
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| DUR (ÀǾàǰ»ç¿ëÆò°¡) |
º´¿ë±Ý±â :
°í½ÃµÈ º´¿ë±Ý±â ³»¿ëÀº ¾ø½À´Ï´Ù.
[»óÈ£ÀÛ¿ë/º´¿ë±Ý±â°Ë»ö]
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| Mechanism of Action |
Latanoprost¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Latanoprost is a prostaglandin F2a analogue. Specifically, Latanoprost is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor. Studies in animals and man suggest that the main mechanism of action is increased uveoscleral outflow. Elevated IOP represents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.
Timolol¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at beta(1)-adrenergic receptors in the heart and vascular smooth muscle and beta(2)-receptors in the bronchial and vascular smooth muscle. Beta(1)-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. Beta(2)-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor.
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| Pharmacology |
Latanoprost¿¡ ´ëÇÑ Pharmacology Á¤º¸ Latanoprost is an isopropyl ester prodrug which is inactive but which becomes active after hydrolysis to the acid from. Latanoprost opthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes.
Timolol¿¡ ´ëÇÑ Pharmacology Á¤º¸ Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage.
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| Protein Binding |
Latanoprost¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Not Available
Timolol¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ ~10%
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| Half-life |
Latanoprost¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 17 minutes
Timolol¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2.5-5 hours
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| Absorption |
Latanoprost¿¡ ´ëÇÑ Absorption Á¤º¸ Latanoprost is well absorbed through the cornea where the isopropyl ester prodrug is hydrolyzed to the acid form. Peak concentration is reached 2 hrs after topical administration.
Timolol¿¡ ´ëÇÑ Absorption Á¤º¸ Bioavailability is about 60%
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| Pharmacokinetics |
Timolol maleateÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Ç÷¾Ð°ÇÏÈ¿°ú ¹ßÇö½Ã°£ : °æ±¸ : 15-45ºÐ À̳»
- ÃÖ°íÈ¿°ú ¹ßÇö½Ã°£ : 0.5-2.5 ½Ã°£
- ÀÛ¿ëÁö¼Ó½Ã°£ : 4½Ã°£±îÁö. Á¡¾È ÈÄ ¾È¾Ð Çϰȿ°ú´Â 24½Ã°£±îÁö Áö¼Ó
- ´Ü¹é°áÇÕ : 60%
- ´ë»ç : ÃÊȸÅë°úÈ¿°ú Å. °£¿¡¼ ¸¹Àº ¾çÀÌ ´ë»çµÊ.
- ¹Ý°¨±â : 2-2.7 ½Ã°£. ½Å±â´ÉºÎÀü½Ã Áõ°¡
- ¼Ò½Ç : ½Å ¹è¼³ (¹Ìº¯Èü·Î¼ 15-20%)
LatanoprostÀÇ ¾à¹°µ¿·ÂÇÐÀÚ·á
- Ä¡·áÈ¿°ú ¹ßÇö½Ã°£ : 3~4½Ã°£
- ÃÖ°í Ç÷Áß³óµµ µµ´Þ½Ã°£ : 8~12½Ã°£
- ¹ÝÀÀ Áö¼Ó ½Ã°£ : 20~23½Ã°£
- Èí¼ö : °¢¸·À» ÅëÇØ Èí¼öµÈ´Ù.
- ºÐÆ÷ ¿ëÀû : 0.16L/kg
- ´ë»ç : ÁÖ·Î °£¿¡¼ ´ë»çµÈ´Ù.
- ¹è¼³ : ½Å¹è¼³ 88~98%
- ¹è¼³ ¹Ý°¨±â : 17ºÐ
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| Biotransformation |
Latanoprost¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic (none except hydrolysis in the eye). Latanoprost is an isopropyl ester prodrug. It is hydrolyzed by esterases in the cornea to latanoprost acid, which is biologically active. The portion of the latanoprost acid that reaches the systemic circulation is metabolized primarily by the liver to 1,2-dinor and 1,2,3,4-tetranor metabolites by fatty acid beta-oxidation.
Timolol¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic (80%) via the cytochrome P450 2D6 isoenzyme.
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| Toxicity |
Latanoprost¿¡ ´ëÇÑ Toxicity Á¤º¸ Symptoms of overdose include bloodshot eyes and eye irritation.
Timolol¿¡ ´ëÇÑ Toxicity Á¤º¸ LD50=1190 mg/kg (oral, mice), LD50=900 mg/kg (oral, rat). Symptoms of overdose include drowsiness, vertigo, headache, and atriventricular block.
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| Drug Interactions |
Latanoprost¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Timolol¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Timolol¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 2D6
Beta Blockers:
S-metoprolol
propafenone
**timolol**
Antidepressants:
amitriptyline
clomipramine
desipramine
imipramine
paroxetine
Antipsychotics:
haloperidol
risperidone
thioridazine
aripiprazole
codeine
dextromethorphan
duloxetine
flecainide
mexiletine
ondansetron
tamoxifen
tramadol
venlafaxine
INHIBITORS
CYP 2D6
amiodarone
buproprion
chlorpheniramine
cimetidine
clomipramine
duloxetine
fluoxetine
haloperidol
methadone
mibefradil
paroxetine
quinidine
ritonavir
INDUCERS
CYP 2D6
N/A
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| Drug Target |
[Drug Target]
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| Description |
Latanoprost¿¡ ´ëÇÑ Description Á¤º¸ Latanoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes.It is also known by the brand name of Xalatan manufactured by Pfizer.
Timolol¿¡ ´ëÇÑ Description Á¤º¸ A beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. It is also used in the treatment of migraine disorders and tremor. [PubChem]
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| Drug Category |
Latanoprost¿¡ ´ëÇÑ Drug_Category Á¤º¸ Antihypertensive AgentsNeuroprotective Agents
Timolol¿¡ ´ëÇÑ Drug_Category Á¤º¸ Adrenergic beta-AntagonistsAnti-Arrhythmia AgentsAntihypertensive Agents
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| Smiles String Canonical |
Latanoprost¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)OC(=O)CCCC=CCC1C(O)CC(O)C1CCC(O)CCC1=CC=CC=C1
Timolol¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ CC(C)(C)NCC(O)COC1=NSN=C1N1CCOCC1
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| Smiles String Isomeric |
Latanoprost¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)OC(=O)CCC\C=C\C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1
Timolol¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ CC(C)(C)NC[C@H](O)COC1=NSN=C1N1CCOCC1
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| InChI Identifier |
Latanoprost¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C26H40O5/c1-19(2)31-26(30)13-9-4-3-8-12-22-23(25(29)18-24(22)28)17-16-21(27)15-14-20-10-6-5-7-11-20/h3,5-8,10-11,19,21-25,27-29H,4,9,12-18H2,1-2H3/b8-3+/t21-,22+,23+,24-,25+/m0/s1
Timolol¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C13H24N4O3S/c1-13(2,3)14-8-10(18)9-20-12-11(15-21-16-12)17-4-6-19-7-5-17/h10,14,18H,4-9H2,1-3H3/t10-/m0/s1
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| Chemical IUPAC Name |
Latanoprost¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ propan-2-yl (E)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2-[(3R)-3-hydroxy-5-phenylpentyl]cyclopentyl]hept-5-enoate
Timolol¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (2S)-1-(tert-butylamino)-3-[(4-morpholin-4-yl-1,2,5-thiadiazol-3-yl)oxy]propan-2-ol
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| Drug-Induced Toxicity Related Proteins |
MALEATE ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:Intercellular adhesion molecule 1 Drug:maleate Toxicity:hepatic injury. [¹Ù·Î°¡±â] TIMOLOL ÀÇ Drug-Induced Toxicity Related ProteinÁ¤º¸ Replated Protein:CYP2D6 Drug:Timolol Toxicity:Increased beta-blockade. [¹Ù·Î°¡±â]
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º» ¼öÁ¤ÀÏ Á¤º¸´Â Çã°¡Á¤º¸ ÀÌ¿ÜÀÇ ±âŸÁ¤º¸ ¼öÁ¤ÀÏÀ» ÀǹÌÇϹǷÎ, Çã°¡Á¤º¸¼öÁ¤ÀÏÀº º»¹®¿¡ Ç¥±âµÈ ³¯Â¥¸¦ ÂüÁ¶ÇϽñ⠹ٶø´Ï´Ù.
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»ó¼¼Á¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×À» Åä´ë·Î ÀÛ¼ºµÇ¾úÀ¸¸ç ¿ä¾àÁ¤º¸´Â »ó¼¼Á¤º¸ ¹× ±âŸ¹®ÇåÀ» ±â¹ÝÀ¸·Î µå·°ÀÎÆ÷¿¡¼ ÆíÁýÇÑ ³»¿ëÀÔ´Ï´Ù. Á¦Ç°Çã°¡»çÇ×ÀÇ ¸ñÂ÷¿Í ´Ù¼Ò »óÀÌÇÒ ¼ö ÀÖ½À´Ï´Ù. |
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°æ°í |
µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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